Simulation of gastric lipolysis and prediction of felodipine release from a matrix tablet in the fed stomach

被引:36
作者
Diakidou, A.
Vertzoni, M.
Abrahamsson, B. [2 ]
Dressman, J. [3 ]
Reppas, C. [1 ]
机构
[1] Univ Athens, Fac Pharm, Lab Biopharmaceut & Pharmacokinet, Zografos 15771, Greece
[2] AstraZeneca R&D, Molndal, Sweden
[3] Univ Frankfurt, Dept Pharmaceut Technol, Frankfurt, Germany
关键词
Intragastric release; Felodipine; Fed state; Biorelevant media; HPMC tablet; VITRO GASTROINTESTINAL MODEL; IN-VITRO; FOLIC-ACID; DISSOLUTION; ABSORPTION; PLASMA; MILK; DISINTEGRATION; PARACETAMOL; LIPASES;
D O I
10.1016/j.ejps.2009.02.003
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The importance of intragastric lipolysis to felodipine release from a hydrophilic, extended release tablet in the fed stomach was assessed in USP II apparatus with the tablet fixed on a steel wire above the paddle. The release medium, homogenized long-life milk. was gradually digested with shots of acidic solutions of pepsin over the course of the experiment in absence and in presence of biorelevant concentrations of a lipase that was similar to human gastric lipase. Percentage tablet erosion at specific times in the same media was measured in separate experiments. The data were compared to published data for intragastric release in fed healthy adults. In all cases, felodipine release occurred under sink conditions. Lipase facilitated felodipine release from the eroded polymer, bringing the release profile closer to the in vivo data. Likewise, the relationship between tablet erosion and amount of released felodipine reflected the in vivo data only when lipase was added to the medium. It was concluded that modelling intragastric lipolysis is necessary in order to simulate felodipine release from the extended release tablets in the fed stomach. (C) 2009 Elsevier B.V. All rights reserved.
引用
收藏
页码:133 / 140
页数:8
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